Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2

Trond Ulven; Michael J Gallen; Mads C Nielsen; Nicole Merten; Carola Schmidt; Klaus Mohr; Christian Tränkle; Evi Kostenis

doi:10.1016/j.bmcl.2007.07.080

Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5924-7. doi: 10.1016/j.bmcl.2007.07.080. Epub 2007 Aug 22.

Authors

Trond Ulven¹, Michael J Gallen, Mads C Nielsen, Nicole Merten, Carola Schmidt, Klaus Mohr, Christian Tränkle, Evi Kostenis

Affiliation

¹ Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.

PMID: 17845848
DOI: 10.1016/j.bmcl.2007.07.080

Abstract

Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Drug Evaluation, Preclinical
Indoles / chemistry
Indoles / pharmacology*
Radioligand Assay
Receptors, Immunologic / antagonists & inhibitors*
Receptors, Prostaglandin / antagonists & inhibitors*
Sulfonamides / chemistry
Sulfonamides / pharmacology*

Substances

Indoles
Receptors, Immunologic
Receptors, Prostaglandin
Sulfonamides
TRQ11238
prostaglandin D2 receptor